The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)



Gene Review

GHSR  -  growth hormone secretagogue receptor

Homo sapiens

Synonyms: GH-releasing peptide receptor, GHRP, GHS-R, Ghrelin receptor, Growth hormone secretagogue receptor type 1
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of GHSR

  • To our knowledge, these data are the first to demonstrate linkage and association of SNPs and haplotypes within the GHSR gene region and human obesity [1].
  • Additionally, the coding region of GHSR was systematically screened, and seven sequence variants were identified in 93 obese, 96 normal weight, and 94 underweight individuals and 43 children with short normal stature (SNS) [2].
  • Body weights of the transgenic mice became similar in adulthood, whereas adipose mass was reduced, particularly so in female GHRH-GHSR mice [3].
  • Ghrelin and growth hormone (GH) secretagogue receptor (GHSR) mRNA expression in human pituitary adenomas [4].
  • The expression of GHSR mRNA was significantly lower in gsp mutation-positive than -negative adenomas [5].

Psychiatry related information on GHSR


High impact information on GHSR

  • They act through the GHS-R, a G protein-coupled receptor whose ligand has only been discovered recently [11].
  • Molecular and genetic models, the discovery of human GHRH and its receptor, the cloning of the GHRP receptor, and the clinical availability of recombinant GH and IGF-I have allowed surprisingly rapid advances in our knowledge of the neuroregulation of the GH-IGF-I axis in many pathophysiological contexts [12].
  • The GHRP receptor has recently been cloned and it does not show sequence homology with other G-protein-coupled receptors known so far [13].
  • This mutation, which results in decreased cell-surface expression of the receptor, selectively impairs the constitutive activity of the GHSR, while preserving its ability to respond to ghrelin [14].
  • The growth hormone (GH) secretagogue receptor (GHSR) was cloned as the target of a family of synthetic molecules endowed with GH release properties [14].

Chemical compound and disease context of GHSR


Biological context of GHSR


Anatomical context of GHSR


Associations of GHSR with chemical compounds

  • The apparent sexual dimorphism in GHSR indicates different regulatory effects of sex steroid in young growing SDRs [20].
  • High doses of GHRP-2 treatment decreased the levels of both GHRH-R and GHS-R mRNA [23].
  • However, non-natural SRIH octapeptide agonists (mainly lanreotide and vapreotide) displace 125I-Tyr-Ala-hexarelin from pituitary binding sites suggesting that an endogenous factor related to SRIH might exist and interact with GHS-R [24].
  • This review will summarize the recent progress in small-molecule GHS-R antagonists and offer some insight into this area of research based on the experience at Abbott Laboratories [25].
  • The constitutive activity of the ghrelin receptor and of neurotensin receptor 2 through the G(q), phospholipase C pathway was approximately 50% of their maximal capacity as determined through inositol phosphate accumulation [26].

Physical interactions of GHSR


Regulatory relationships of GHSR


Other interactions of GHSR


Analytical, diagnostic and therapeutic context of GHSR


  1. Genetic linkage and association of the growth hormone secretagogue receptor (ghrelin receptor) gene in human obesity. Baessler, A., Hasinoff, M.J., Fischer, M., Reinhard, W., Sonnenberg, G.E., Olivier, M., Erdmann, J., Schunkert, H., Doering, A., Jacob, H.J., Comuzzie, A.G., Kissebah, A.H., Kwitek, A.E. Diabetes (2005) [Pubmed]
  2. Ghrelin receptor gene: identification of several sequence variants in extremely obese children and adolescents, healthy normal-weight and underweight students, and children with short normal stature. Wang, H.J., Geller, F., Dempfle, A., Schäuble, N., Friedel, S., Lichtner, P., Fontenla-Horro, F., Wudy, S., Hagemann, S., Gortner, L., Huse, K., Remschmidt, H., Bettecken, T., Meitinger, T., Schäfer, H., Hebebrand, J., Hinney, A. J. Clin. Endocrinol. Metab. (2004) [Pubmed]
  3. Physiological studies of transgenic mice overexpressing growth hormone (GH) secretagogue receptor 1A in GH-releasing hormone neurons. Lall, S., Balthasar, N., Carmignac, D., Magoulas, C., Sesay, A., Houston, P., Mathers, K., Robinson, I. Endocrinology (2004) [Pubmed]
  4. Ghrelin and growth hormone (GH) secretagogue receptor (GHSR) mRNA expression in human pituitary adenomas. Kim, K., Arai, K., Sanno, N., Osamura, R.Y., Teramoto, A., Shibasaki, T. Clin. Endocrinol. (Oxf) (2001) [Pubmed]
  5. Ghrelin mRNA and GH secretagogue receptor mRNA in human GH-producing pituitary adenomas is affected by mutations in the alpha subunit of G protein. Kim, K., Sanno, N., Arai, K., Takano, K., Yasufuku-Takano, J., Teramoto, A., Shibasaki, T. Clin. Endocrinol. (Oxf) (2003) [Pubmed]
  6. Circulating ghrelin levels and central ghrelin receptor expression are elevated in response to food deprivation in a seasonal mammal (Phodopus sungorus). Tups, A., Helwig, M., Khorooshi, R.M., Archer, Z.A., Klingenspor, M., Mercer, J.G. J. Neuroendocrinol. (2004) [Pubmed]
  7. The endocrine response to acute ghrelin administration is blunted in patients with anorexia nervosa, a ghrelin hypersecretory state. Broglio, F., Gianotti, L., Destefanis, S., Fassino, S., Abbate Daga, G., Mondelli, V., Lanfranco, F., Gottero, C., Gauna, C., Hofland, L., Van der Lely, A.J., Ghigo, E. Clin. Endocrinol. (Oxf) (2004) [Pubmed]
  8. Effects of central infusion of ghrelin on food intake and plasma levels of growth hormone, luteinizing hormone, prolactin, and cortisol secretion in sheep. Iqbal, J., Kurose, Y., Canny, B., Clarke, I.J. Endocrinology (2006) [Pubmed]
  9. Sleep enhances nocturnal plasma ghrelin levels in healthy subjects. Dzaja, A., Dalal, M.A., Himmerich, H., Uhr, M., Pollmächer, T., Schuld, A. Am. J. Physiol. Endocrinol. Metab. (2004) [Pubmed]
  10. Neuroendocrine and peripheral activities of ghrelin: implications in metabolism and obesity. Muccioli, G., Tschöp, M., Papotti, M., Deghenghi, R., Heiman, M., Ghigo, E. Eur. J. Pharmacol. (2002) [Pubmed]
  11. Ghrelin: structure and function. Kojima, M., Kangawa, K. Physiol. Rev. (2005) [Pubmed]
  12. Pathophysiology of the neuroregulation of growth hormone secretion in experimental animals and the human. Giustina, A., Veldhuis, J.D. Endocr. Rev. (1998) [Pubmed]
  13. Growth hormone-releasing peptides and their analogs. Camanni, F., Ghigo, E., Arvat, E. Frontiers in neuroendocrinology. (1998) [Pubmed]
  14. Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature. Pantel, J., Legendre, M., Cabrol, S., Hilal, L., Hajaji, Y., Morisset, S., Nivot, S., Vie-Luton, M.P., Grouselle, D., de Kerdanet, M., Kadiri, A., Epelbaum, J., Le Bouc, Y., Amselem, S. J. Clin. Invest. (2006) [Pubmed]
  15. Estradiol-dependent decrease in the orexigenic potency of ghrelin in female rats. Clegg, D.J., Brown, L.M., Zigman, J.M., Kemp, C.J., Strader, A.D., Benoit, S.C., Woods, S.C., Mangiaracina, M., Geary, N. Diabetes (2007) [Pubmed]
  16. NPY/AgRP neurons are not essential for feeding responses to glucoprivation. Luquet, S., Phillips, C.T., Palmiter, R.D. Peptides (2007) [Pubmed]
  17. The role of the GH/IGF-I axis for cardiac function and structure. Isgaard, J., Tivesten, A., Friberg, P., Bengtsson, B.A. Horm. Metab. Res. (1999) [Pubmed]
  18. Potential role of new therapies in modifying cardiovascular risk in overweight patients with metabolic risk factors. Jensen, M.D. Obesity (Silver Spring, Md.) (2006) [Pubmed]
  19. Obestatin partially affects ghrelin stimulation of food intake and growth hormone secretion in rodents. Zizzari, P., Longchamps, R., Epelbaum, J., Bluet-Pajot, M.T. Endocrinology (2007) [Pubmed]
  20. Regulation of pituitary growth hormone-secretagogue and growth hormone-releasing hormone receptor RNA expression in young Dwarf rats. Horikawa, R., Tachibana, T., Katsumata, N., Ishikawa, H., Tanaka, T. Endocr. J. (2000) [Pubmed]
  21. Ghrelin and the growth hormone secretagogue receptor constitute a novel autocrine pathway in astrocytoma motility. Dixit, V.D., Weeraratna, A.T., Yang, H., Bertak, D., Cooper-Jenkins, A., Riggins, G.J., Eberhart, C.G., Taub, D.D. J. Biol. Chem. (2006) [Pubmed]
  22. Ghrelin in fetal thyroid and follicular tumors and cell lines: expression and effects on tumor growth. Volante, M., Allia, E., Fulcheri, E., Cassoni, P., Ghigo, E., Muccioli, G., Papotti, M. Am. J. Pathol. (2003) [Pubmed]
  23. Differential Regulation of GHRH-Receptor and GHS-Receptor Expression by Long-Term In Vitro Treatment of Ovine Pituitary Cells with GHRP-2 and GHRH. Roh, S.G., Doconto, M., Feng, D.D., Chen, C. Endocrine (2006) [Pubmed]
  24. Cortistatin, but not somatostatin, binds to growth hormone secretagogue (GHS) receptors of human pituitary gland. Deghenghi, R., Papotti, M., Ghigo, E., Muccioli, G. J. Endocrinol. Invest. (2001) [Pubmed]
  25. Growth hormone secretagogue receptor antagonists as anti-obesity therapies? Still an open question. Zhao, H., Liu, G. Current opinion in drug discovery & development. (2006) [Pubmed]
  26. Common structural basis for constitutive activity of the ghrelin receptor family. Holst, B., Holliday, N.D., Bach, A., Elling, C.E., Cox, H.M., Schwartz, T.W. J. Biol. Chem. (2004) [Pubmed]
  27. Characterization of ghrelin receptor activity in a rat pituitary cell line RC-4B/C. Falls, H.D., Dayton, B.D., Fry, D.G., Ogiela, C.A., Schaefer, V.G., Brodjian, S., Reilly, R.M., Collins, C.A., Kaszubska, W. J. Mol. Endocrinol. (2006) [Pubmed]
  28. Growth hormone (GH)-releasing peptide stimulation of GH release from human somatotroph adenoma cells: interaction with GH-releasing hormone, thyrotropin-releasing hormone, and octreotide. Renner, U., Brockmeier, S., Strasburger, C.J., Lange, M., Schopohl, J., Müller, O.A., von Werder, K., Stalla, G.K. J. Clin. Endocrinol. Metab. (1994) [Pubmed]
  29. Brainstem Thyrotropin-Releasing Hormone Regulates Food Intake through Vagal-Dependent Cholinergic Stimulation of Ghrelin Secretion. Ao, Y., Go, V.L., Toy, N., Li, T., Wang, Y., Song, M.K., Reeve, J.R., Liu, Y., Yang, H. Endocrinology (2006) [Pubmed]
  30. Expression of functional growth hormone secretagogue receptors in human pituitary adenomas: polymerase chain reaction, triple in-situ hybridization and cell culture studies. Barlier, A., Zamora, A.J., Grino, M., Gunz, G., Pellegrini-Bouiller, I., Morange-Ramos, I., Figarella-Branger, D., Dufour, H., Jaquet, P., Enjalbert, A. J. Neuroendocrinol. (1999) [Pubmed]
  31. Cloning and characterization of two human G protein-coupled receptor genes (GPR38 and GPR39) related to the growth hormone secretagogue and neurotensin receptors. McKee, K.K., Tan, C.P., Palyha, O.C., Liu, J., Feighner, S.D., Hreniuk, D.L., Smith, R.G., Howard, A.D., Van der Ploeg, L.H. Genomics (1997) [Pubmed]
  32. Growth hormone secretagogue receptor family members and ligands. Smith, R.G., Leonard, R., Bailey, A.R., Palyha, O., Feighner, S., Tan, C., Mckee, K.K., Pong, S.S., Griffin, P., Howard, A. Endocrine (2001) [Pubmed]
  33. Expression of ghrelin and biological activity of specific receptors for ghrelin and des-acyl ghrelin in human prostate neoplasms and related cell lines. Cassoni, P., Ghé, C., Marrocco, T., Tarabra, E., Allia, E., Catapano, F., Deghenghi, R., Ghigo, E., Papotti, M., Muccioli, G. Eur. J. Endocrinol. (2004) [Pubmed]
WikiGenes - Universities